CP 481715
| CAS号 | 212790-31-3 | 货号 | BCP18399 |
| 中文名 | CP 481715 | ||
| 英文名 | CP 481715 | ||
| 中文别名 | |||
| 英文别名 | CP-481715;CP481715; CP-481,715; CP 481,715; CP481,71; | ||
| 分子式 | C26H31FN4O4 | 分子量 | 482.55 |
| 生物活性 | CP 481715 a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. CP-481,715 binds to human CCR1 with a Kd of 9.2 nm. and displaces 125I-labeled CCL3 from CCR1-transfected cells with an IC50 of 74 nm. CP-481,715 fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (guanosine 5'-O-(thiotriphosphate) incorporation; IC50 = 210 nm), calcium mobilization (IC50 = 71 nm), monocyte chemotaxis (IC50 = 55 nm), and matrix metalloproteinase 9 release (IC50 = 54 nm). CP-481,715 retains activity in human whole blood, inhibiting CCL3-induced CD11b up-regulation and actin polymerization (IC50 = 165 and 57 nm, respectively) on monocytes. CP-481,715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice. | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | CCR | ||
结构式
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